Composition for oral cavity

ABSTRACT

The present invention provides an oral composition comprising crystalline cellulose, and one or more surface active agents selected from the group consisting of alkyl glycoside, polyglycerin fatty acid ester, sucrose fatty acid ester and betaine, which has an excellent shape-holding ability and dispersibility in an oral cavity, does not change a taste of juice after teeth brushing, in addition, has excellent stability with time not causing solid-liquid separation. Moreover, the present invention provides an oral composition comprising a cationic bactericide and crystalline cellulose, which can effectively prevent an oral cavity disease such as a periodontal disease, dental caries and the like by enhancing an ability of the cationic bactericide to reside on a tooth surface.

BACKGROUND OF THE INVENTION

1. Field of the Invention

The present invention relates to an oral composition which has anexcellent shape-holding ability and dispersibility, and does not changea taste of juice after teeth brushing and, particularly, has excellentstability with time. Moreover, the present invention relates to an oralcomposition having an excellent ability of a cationic bactericide toreside on a tooth surface.

2. Description of the Related Art

Hitherto, a shape-holding ability and dispersibility in an oral cavityof an oral composition have been obtained by containing therein athickening agent, which is generally and frequently used, such ascarboxymethyl cellulose, methyl cellulose, hydroxyethyl cellulose, gumarabic, xanthan gum, carrageenan, sodium alginate, sodium polyacrylateand the like. In addition, an oral composition having bettershape-holding ability and dispersibility in an oral cavity than those ofprior art, which is prepared by containing therein finely-dividedcellulose, has been proposed in JPA 58861/1993. However, such the oralcomposition has practical problems such as occurrence of solid-liquidseparation during long term storage. In addition, in such the oralcomposition, sodium alkylsulfate is used as a surface active agent,which is known to change a taste of juice after teeth brushing.

On the other hand, a cationic bactericide is contained in various oralcompositions in order to prevent an oral cavity disease such as aperiodontal disease, dental caries and the like, because it has anexcellent ability to be adsorbed to an oral tissue, an enhancedbactericidal activity and an enhanced plaque formation-suppressingeffect.

However, there was a problem that, since the cationic bactericide has anelectric charge, it forms an electrostatic complex with other anionicingredients contained in the oral composition, and a bactericidalactivity per unit of the cationic bactericide is reduced. In responsethereto, attempts have been conducted to prevent reduction of theactivity per unit of the cationic bactericide, by containing a nonionicor amphoteric surface active agent or a nonionic thickening agent in theoral compositions, but sufficient effects have not been obtained yet.

On the other hand, even the cationic bactericide exhibits a transientbactericidal effect in many cases, and it is contemplated that anactivity of the bactericide can be totally enhanced by improving anability of the cationic bactericide to reside on a tooth surface.

BRIEF SUMMARY OF THE INVENTION

A first object of the present invention is to provide an oralcomposition which retains better shape-holding ability, is excellent indispersibility in an oral cavity, does not change a taste of juice afterteeth brushing, and does not cause solid-liquid separation during longterm storage and, additionally, which has an improved ability of thecationic bactericide to reside on a tooth surface.

Moreover, a second object of the present invention is to provide an oralcomposition which can effectively prevent a periodontal disease anddental caries by enhancing the ability of a cationic bactericide toreside on a tooth surface to enhance a residence bactericidal activityof the cationic bactericide.

In view of above former situations, the present inventors studiedintensively, and found that an oral composition which has an excellentshape-holding ability and dispersibility in an oral cavity, does notchange a taste of juice after teeth brushing, and does not causesolid-liquid separation during long term storage, can be obtained bycontaining a combination of crystalline cellulose and a particularsurface active agent, which resulted in completion of a first aspect ofthe present invention.

Moreover, in view of above latter situations, the present inventorsstudied intensively, and found that the ability of the cationicbactericide to reside on a tooth surface is significantly enhanced bycontaining a specific combination of the cationic bactericide andcrystalline cellulose, which resulted in completion of a second aspectof the present invention.

That is, in accordance with the first aspect, the present inventionprovides:

-   -   1. An oral composition comprising crystalline cellulose, and one        or more surface active agents selected from the group consisting        of alkyl glycoside, polyglycerin fatty acid ester, sucrose fatty        acid ester and betaine;    -   2. The oral composition of according to (1), wherein the        crystalline cellulose is contained at 0.2-10% by weight;    -   3. The oral composition according to (1) or (2), wherein the        surface active agent is alkyl glycoside;    -   4. The oral composition according to (3), wherein an alkyl chain        of the alkyl glycoside is C8-C16 in length;    -   5. The oral composition according to (1) or (2), wherein the        surface active agent is polyglycerin fatty acid ester or sucrose        fatty acid ester;    -   6. The oral composition according to (5), wherein an alkyl chain        of a fatty acid portion of the polyglycerin fatty acid ester or        the sucrose fatty acid ester is C8-C16 in length;    -   7. The oral composition according to (1) or (2), wherein the        surface active agent is betaine;    -   8. The oral composition according to (7), wherein the betaine is        fatty acid amide propyl betaine;    -   9. The oral composition according to (8), wherein an alkyl chain        of a fatty acid portion of the fatty acid amide propyl betaine        is C8-C16 in length; and    -   10. The oral composition according to any one of (1)-(9),        further comprising a cationic bactericide.

According to the first aspect of the present invention, an oralcomposition can be provided, which has an excellent shape-holdingability and dispersibility in an oral cavity, does not change a taste ofjuice after teeth brushing and, particularly, has excellent stabilitywith time, or additionally has an enhanced ability of the cationicbactericide to reside on a tooth surface in addition to abovecharacteristics.

Moreover, in accordance with the second aspect, the present inventionprovides:

-   -   11. An oral composition comprising a cationic bactericide and        crystalline cellulose;    -   12. The oral composition according to (11), wherein the cationic        bactericide is a quaternary ammonium salt;    -   13. The oral composition according to (11), wherein the cationic        bactericide is a biguanide bactericide;    -   14. The oral composition according to (11), wherein the cationic        bactericide is one or more selected from the group consisting of        cetylpyridinium chloride, benzalkonium chloride, benzethonium        chloride, chlorhexidine hydrochloride and chlorhexidine        gluconate;    -   15. The oral composition according to any one of (11)-(14),        wherein the cationic bactericide is contained at 0.001-10% by        weight;    -   16. The oral composition according to any one of (11)-(15),        wherein the crystalline cellulose is contained at 0.2-10% by        weight;    -   17. The oral composition according to any one of (11)-(16),        further comprising one or more surface active agents selected        from nonionic and amphoteric surface active agents;    -   18. The oral composition according to (17), wherein the surface        active agent is alkyl glycoside having an alkyl chain of C8-C16        in length; and    -   19. The oral composition according to (17), wherein the surface        active agent is fatty acid amide propyl betaine having an alkyl        chain of a fatty acid portion of C8-C16 in length.

According to the second aspect of the present invention, an oralcomposition can be provided, which can significantly enhance the effectof the cationic bactericide to reside on the tooth surface andeffectively prevent the oral cavity disease such as the periodontaldisease, dental caries and the like.

DETAILED DESCRIPTION OF THE INVENTION

The first and second aspects of the present invention are sequentiallyillustrated below.

Crystalline cellulose used in the first aspect of the present inventionis not particularly limited as far as it is commercially available, butcrystalline cellulose having an average particle diameter of 10micrometer or smaller is more preferable and crystalline cellulosehaving an average particle diameter of 2-6 micrometer is mostpreferable. When the average particle diameter of crystalline celluloseis larger than 10 micrometer, dispersibility of the oral composition inthe oral cavity is deteriorated. In addition, an amount of crystallinecellulose to be contained is preferably 0.2-10% by weight based on atotal weight of the oral composition. When the amount of crystallinecellulose is smaller than 0.2% by weight, an adequate shape-holdingability of the oral composition can not be achieved, being is notpreferable. On the other hand, when the amount of crystalline celluloseis larger than 10% by weight, a viscosity of the oral compositionbecomes too high, being not preferable.

The surface active agent used in the first aspect of the presentinvention includes alkyl glycoside, polyglycerin fatty acid ester,sucrose fatty acid ester and betaine, and they may be used alone or in acombination of two or more. An amount of the surface active agent to becontained is preferably 0.5-5% by weight based on a total weight of theoral composition. When the amount of the surface active agent to becontained is smaller than 0.5% by weight, a foaming ability of the oralcomposition is reduced, and a use feeling is deteriorated, being notpreferable. On the other hand, when the amount of the surface activeagent to be contained is larger than 5% by weight, a taste or a smellderived from the surface active agent becomes unnegligible, being notpreferable.

Among above surface active agents, alkyl glycoside used in the presentinvention is not particularly limited, but an alkyl chain thereof ispreferably C8-C16 in length. When the alkyl chain is shorter than C8, abitter taste is produced in the oral composition, being not preferable.On the other hand, when the alkyl chain is longer than C16, the foamingability of the oral composition is lowered and it becomes uncomfortableto use in some cases, being not preferable. Examples within such thechain length range include decyl glycoside, lauryl glycoside, myristylglycoside and the like, and PLANTACARE 1200, PLANTACARE 2000 (Cognis),Oramix NS10, Oramix NS26 (SEPPIC) and the like are commerciallyavailable.

In addition, polyglycerin fatty acid ester used in the first aspect ofthe present invention is not particularly limited, but an alkyl chain ofa fatty acid portion thereof is preferably C8-C16 in length. When thealkyl chain is shorter than C8, a bitter taste is produced in the oralcomposition. On the other hand, when the alkyl chain is longer than C16,there is a tendency that the foaming ability of the oral composition islowered. In addition, a polymerization degree of a polyglycerin portionis preferably equal to or greater than 4. When the polymerization degreeis equal to or smaller than 3, there is a tendency that the foamingability of the oral composition is lowered. Examples of suchpolyglycerin fatty acid ester include decaglycerin monolauric acidester, tetraglycerin monolauric acid ester, decaglycerin monomyristicacid ester, tetraglycerin monomyristic acid ester and the like, andNIKKOL Decaglyn 1-L, NIKKOL Tetraglyn 1-L, NIKKOL Decaglyn 1-M (NikkoChemicals, Co., Ltd.), Sunsoft Q-12W, Sunsoft Q-12T, Sunsoft Q-14W(Taiyo Kagaku Co., Ltd.) and the like are commercially available.

In addition, sucrose fatty acid ester used in the first aspect of thepresent invention is not particularly limited, but an alkyl chain of afatty acid portion thereof is preferably C8-C16 in length. When thealkyl chain is shorter than C8, a bitter taste is produced in the oralcomposition. On the other hand, when the alkyl chain is longer than C16,the foaming ability of the oral composition is lowered and an oily tasteis produced in some cases in the oral composition. Examples of suchsucrose fatty acid ester include sucrose lauric acid ester, sucrosepalmitic acid ester and the like, and DK ester S series (Daiichi KogyoSeiyaku Co., Ltd.), Ryoto sugar ester (Mitsubishi Kagaku Foods Co.) andthe like are commercially available.

In addition, the betaine surface active agent used in the first aspectof the present invention is not particularly limited, but examplesthereof include alkyl betaine, fatty acid amide propyl betaine, alkylsulfobetaine, imidazolinium betaine and the like. Among them, fatty acidamide propyl betaine is preferable in view of its weak bitter taste. Inaddition, an alkyl chain of a fatty acid portion of fatty acid amidepropyl betaine is preferably C8-C16 in length. When the alkyl chain isshorter than C8, a bitter taste is produced in the oral composition. Onthe other hand, when the alkyl chain is longer than C16, the foamingability of the oral composition is lowered and an oily taste is producedin some cases in the oral composition. Examples of fatty acid amidepropyl betaine having such the chain length range include coconut oilfatty acid amide propyl betaine, lauric acid amide propyl betaine,myristic acid amide propyl betaine and the like, and there arecommercially available products such as SWANOL (Nikko Chemicals, Co.,Ltd.), Obazolin (Toho Chemical Industry Co., Ltd.), RIKABION (New JapanChemical Co., Ltd.), Tego-Betaine (Goldschmidt AG), Empigen (Albright &Wilson) and the like.

In addition, a cationic bactericide used in the first aspect of thepresent invention is not particularly limited, but a quaternary ammoniumsalt and a biguanide bactericide are preferable, and examples thereofinclude, for example, the quaternary ammonium salt such ascetylpyridinium chloride, benzalkonium chloride, benzethonium chloride,distearyldimethyl ammonium chloride, stearyldimethylbenzyl ammoniumchloride, stearyltrimethyl ammonium chloride, cetyltrimethyl ammoniumchloride, lauryltrimethyl ammonium chloride, laurylpyridinium chlorideand the like, and the biguanide bactericide such as chlorhexidinehydrochloride, chlorhexidine acetate, chlorhexidine gluconate, alexidinhydrochloride, alexidin acetate, alexidin gluconate and the like, andthe like. Among them, cetylpyridinium chloride and benzalkonium chlorideare more preferable, and cetylpyridinium chloride is particularlypreferable. These cationic bacrtericides may be contained alone or in acombination of two or more. In addition, an mount of the cationicbactericide to be contained is preferably 0.001-10% by weight, and morepreferably 0.01-1% by weight based on a total weight of the oralcomposition. When the amount of the cationic bactericide is smaller than0.001% by weight, a bactericidal effect of the oral composition can notbe expected. On the other hand, when the amount of the cationicbactericide is larger than 10% by weight, an irritation to an oralmucous membrane becomes strong, being not preferable in view of safety.

The oral composition of the first aspect of the present invention can beprepared in a form of toothpaste, wet dentifrices, liquid dentifrices,oral paste, gels, sprays, foams and the like. Ingredients, for example,active ingredients, foaming agents or detergents, polishing agents,thickening agents, humectants, preservatives, flavors, sweeteners, pHadjusting agents or the like may be properly contained in the oralcomposition of the first aspect of the present invention as far as theydo not deteriorate the effects of the present invention, depending on adifference in the form of the oral composition.

Among them, examples of the active ingredient include a nonionicbactericide such as triclosan, isopropyl methylphenol and the like, afluoride such as sodium fluoride, potassium fluoride, ammonium fluoride,tin fluoride, sodium monofluorophosphate and the like, an enzyme such asamylase, protease, lysozyme, dextranase and the like, a vitamin such asvitamins B, C and E and the like, a potassium salt and the like.

Examples of the foaming agent or detergent include an anionic surfaceactive agent such as sodium N-acyl sarcosinate, N-acyl glutamate, sodiumN-methyl-N-acyltaurine, sodium N-methyl-N-acylalanine, sodiumalpha-olefin sulfonate and the like; a nonionic surface active agentsuch as polyoxyethylene fatty acid ester such as polyoxyethylenesorbitan fatty acid ester such as polyoxyethylene sorbitan monolaurate,or polyoxyethylene hydrogenated castor oil, lauric acid monoethanolamide, myristic acid monoethanol amide, polyoxyethylene higheralcohol-ether, polyoxyethylene(polyoxypropylene)copolymer,polyoxyethylene(polyoxypropylene)fatty acid ester and the like; anamphoteric surface active agent such as N-alkyldiamino ethyl glycine andthe like, in addition to the surface active agents as described above.But, when the oral composition of the first aspect of the presentinvention contains the cationic bactericide, it is not preferable thatit contains the anionic surface active agent.

Examples of the polishing agent include calcium hydrogenphosphatedihydrate or anhydrate, calcium phosphate, calcium tertiary phosphate,magnesium tertiary phosphate, calcium pyrophosphate, hydroxyapatite,insoluble sodium metaphosphate, silicic acid hydrate, silicic acidanhydrate, silica gel, precipitated silica, aluminum silicate, zirconiumsilicate, calcium silicate, calcium carbonate, magnesium carbonate,alumina, aluminum hydroxide, calcium sulfate, methyl polymethacrylateand the like.

Examples of the thickening agent include an anionic thickening agentsuch as sodium carboxymethyl cellulose, sodium carboxymethylhydroxyethyl cellulose and the like, a cellulose derivative such ashydroxyethyl cellulose, hydroxypropyl cellulose and the like, naturalgum such as xanthan gum, tragacanth, gum karaya, gum arabic, carrageenanand the like, a cationic thickening agent such asO-[2-hydroxy-3-(trimethylammonio)propyl]hydroxyethyl cellulose chlorideand the like, in addition to crystalline cellulose used in the presentinvention. But, when the oral composition of the first aspect of thepresent invention contains the cationic bactericide, it is notpreferable that it contains the anionic thickening agent.

Examples of the humectant include glycerin, propylene glycol,1,3-butylene glycol, sorbitol, polyethylene glycol, xylitol,polypropylene glycol and the like.

Examples of the preservative include paraoxybenzoic acid ester such asmethyl paraben, propyl paraben and the like, benzoate, sodium benzoateand the like.

Examples of the flavor include menthol, carvone, eugenol, methylsalicylate, methyl eugenol, thymol, anethole, limonene, ocimene, n-decylalcohol, citronel, alpha-terpineol, methyl acetate, citronenyl acetate,cinneole, linalool, ethyl linalool, vanillin, thyme, nutmeg, spearmintoil, peppermint oil, lemon oil, orange oil, sage oil, rosemary oil,cinnamon oil, perilla oil, wintergreen oil, cloves oil, eucalyptus oil,piment oil, tea tree oil, Davana oil and the like.

Examples of the sweetener include saccharin sodium, acesulfamepotassium, stevioside, neohesperidin dihydrochalcone, glycyrrhizin,perillartine, thaumatin, aspartyl phenylalanine methyl ester,methoxycinnamic aldehyde, xylit and the like.

Examples of the pH-adjusting agent include citric acid, phosphoric acid,malic acid, gluconic acid, maleic acid, aspartic acid, gluconic acid,succinic acid, glucuronic acid, fumaric acid, glutamic acid, adipic acidand salts thereof, hydrochloric acid, sodium hydroxide, potassiumhydroxide, sodium silicate and the like.

These ingredients may be contained alone or in a combination of two ormore in the oral composition of the first aspect of the presentinvention.

Next, the cationic bactericide used in the second aspect of the presentinvention is not particularly limited, but a quaternary ammonium saltand a biguanide bactericide are preferable, and examples thereofinclude, for example, the quaternary ammonium salt such ascetylpyridinium chloride, benzalkonium chloride, benzethonium chloride,distearyldimethyl ammonium chloride, stearyldimethylbenzyl ammoniumchloride, stearyltrimethyl ammonium chloride, cetyltrimethyl ammoniumchloride, lauryltrimethyl ammonium chloride, laurylpyridinium chlorideand the like, and the biguanide bactericide such as chlorhexidinehydrochloride, chlorhexidine acetate, chlorhexidine gluconate, alexidinhydrochloride, alexidin acetate, alexidin gluconate and the like, andthe like. These cationic bactericides may be contained alone or in acombination of two or more. In addition, an amount of the cationicbactericide to be contained is preferably 0.001-10% by weight and morepreferably 0.01-1% by weight based on a total weight of the oralcomposition. When the amount of the cationic bactericide is smaller than0.001% by weight, an expected bactericidal effect is not exerted. On theother hand, when the amount of the cationic bactericide is larger than10% by weight, an irritation to an oral mucous membrane becomes strong,being not preferable in view of safety.

In addition, crystalline cellulose used in the second aspect of thepresent invention is not particularly limited as far as it iscommercially available. An amount of crystalline cellulose to becontained is preferably 0.2-10% by weight and more preferably 0.5-5% byweight based on a total weight of the oral composition. When the amountof crystalline cellulose is smaller than 0.2% by weight, an effect forenhancing residence of the bactericide on a tooth surface is lowered. Onthe other hand, when the amount of crystalline cellulose is larger than10% by weight, a viscosity of the oral composition becomes too high,being not preferable. In addition, an average particle diameter ofcrystalline cellulose is preferably equal to or smaller than 10micrometer and more preferably 2-6 micrometer, in view of homogeneousdispersion in the oral composition. In addition, as a matter of fact,crystalline cellulose having an average particle diameter smaller than0.1 micrometer is hard to obtain.

In addition, the surface active agent used in the second aspect of thepresent invention is preferably a nonionic surface active agent, anamphoteric surface active agent or a cationic surface active agent. Whenthe anionic surface active agent is used in the oral composition of thepresent invention, stability of the cationic bactericide in aformulation may be deteriorated. More preferably, the surface activeagent is the nonionic and amphoteric surface active agents. Examples ofthe nonionic surface active agent include, for example, sugar fatty acidester such as alkyl glycoside, sucrose fatty acid ester, maltose fattyacid ester, lactose fatty acid ester and the like, polyoxyethylene alkylether, fatty acid alkanol amide, polyoxyethylene sorbitan fatty acidester such as polyoxyethylene sorbitan monolaurate, polyoxyethylenesorbitan monostearate and the like, polyoxyethylene hydrogenated castoroil, sorbitan fatty acid ester, polyglycerin fatty acid ester such asdecaglycerin monolauric acid ester, pentaglycerin distearic acid esterand the like, polyoxyethylene(polyoxypropylene)copolymer, and the like.Examples of the amphoteric surface active agent include, for example,N-alkyldiamino ethyl glycine such as N-lauryldiamino ethyl glycine,N-myristyl dimino ethyl glycine and the like, fatty acid amide propylbetaine, N-alkyl-N-carboxymethyl ammonium betaine, sodium2-alkyl-1-hydroxyethyl imidazoline betaine and the like. Among them,alkyl glycoside, sucrose fatty acid ester polyoxyethylene hydrogenatedcaster oil, polyglycerin fatty acid ester, polyoxyethylene(polyoxypropylene) copolymer, N-alkyl diamino ethyl glycine and fattyacid amide propyl betaine are preferable. Among them, alkyl glycosideand fatty acid amide propyl betaine are particularly preferable. Inaddition, an alkyl chain of alkyl glycoside of C8-C16 in length ispreferable, and an alkyl chain of alkyl glycoside of C10-C14 in lengthis particularly preferable. In addition, an alkyl chain of a fatty acidportion of fatty acid amide propyl betaine is preferably C10-C14 inlength, and particularly C12-C14 in length. An amount of the surfaceactive agent to be contained is preferably 0.5-5% by weight based on atotal weight of the oral composition.

The oral composition of the second aspect of the present invention canbe prepared in a form of toothpaste, wet dentifrices, liquiddentifrices, oral paste, gels and the like. Ingredients, for example,active ingredients, polishing agents, thickening agents, humectants,preservatives, flavors, sweeteners, pH adjusting agents or the like maybe properly contained in the oral composition of the second aspect ofthe present invention as far as they do not deteriorate the effects ofthe present invention, depending on a difference in the form of the oralcomposition.

Among them, examples of the active ingredient include a nonionicbactericide such as triclosan, isopropyl methylphenol and the like, afluoride such as sodium fluoride, potassium fluoride, ammonium fluoride,tin fluoride, sodium monofluorophosphate and the like, an enzyme such asamylase, protease,_lysozyme, dextranase and the like, a vitamin such asvitamins B, C and E and the like, an astringent such as potassiumnitrate, aluminum lactate and the like, and the like, in addition to thecationic bactericide such as the quaternary ammonium salt and thebiguanide bactericide as described above.

Examples of the polishing agent include calcium hydrogenphosphate,dihydrate and anhydrate, calcium phosphate, calcium tertiary phosphate,magnesium tertiary phosphate, calcium pyrophosphate, hydroxyapatite,insoluble sodium metaphosphate, silicic acid hydrate, silicic acidanhydrate, silica gel, precipitated silica, aluminum silicate, zirconiumsilicate, calcium silicate, calcium carbonate, magnesium carbonate,alumina, aluminum hydroxide, calcium sulfate, methyl polymethacrylateand the like. Among them, calcium hydrogenphosphate, dihydrate andanhydrate, calcium phosphate, calcium tertiary phosphate, magnesiumtertiary phosphate, calcium pyrophosphate, hydroxyapatite, calciumcarbonate and magnesium carbonate are preferable.

Examples of the thickening agent include a cellulose derivative such ashydroxyethyl cellulose, hydroxypropyl cellulose and the like, a naturalgum such as carrageenan, xanthan gum, tragacanth, gum karaya, gumarabic, gellan gum and the like, a synthetic thickening agent such aspoly(vinylalcohol), sodium polyacrylate and the like, an inorganicthickening agent such as viscosity-increasing silica, veegum and thelike, and the like, in addition to crystalline cellulose used in theoral composition of the present invention.

Examples of the humectant include glycerin, ethylene glycol, propyleneglycol, 1,3-butylene glycol, polyethylene glycol, polypropylene glycol,sorbit, xylit, maltit, lactit, palatinit and the like.

Examples of the preservative include paraoxybenzoic acid ester such asmethyl paraben, propyl paraben and the like, benzoate, sodium benzoateand the like.

Examples of the flavor include menthol, carvone, eugenol, methylsalicylate, methyl eugenol, thymol, anethole, limonene, ocimene, n-decylalcohol, citronel, alpha-terpineol, methyl acetate, citronenyl acetate,cinneole, linalool, ethyl linalool, vanil in, thyme, nutmeg, spearmintoil, peppermint oil, lemon oil, orange oil, sage oil, rosemary oil,cinnamon oil, perilla oil, wintergreen oil, cloves oil, eucalyptus oil,piment oil, tea tree oil, Davana oil and the like.

Examples of the sweetener include saccharin sodium, acesulfamepotassium, stevioside, neohesperidin dihydrochalcone, glycyrrhizin,perillartine, thaumatin, aspartyl phenylalanine methyl ester,methoxycinnamic aldehyde, xylit and the like.

Examples of the pH-adjusting agent include citric acid, phosphoric acid,malic acid, gluconic acid, maleic acid, aspartic acid, gluconic acid,succinic acid, glucuronic acid, fumaric acid, glutamic acid, adipic acidand salts thereof, hydrochloric acid, sodium hydroxide, potassiumhydroxide, sodium silicate and the like.

These ingredients may be contained alone or in a combination of two ormore in the oral composition of the second aspect of the presentinvention.

EXAMPLES

The first and second aspects of the present invention will be furtherillustrated in detail by referring to the following Examples, but thepresent invention is not limited to such the Examples. In the Examples,the term “%” means “% by weight”, unless otherwise indicated.

Each oral composition of the present invention was prepared according tothe formulation shown in Table 1 by conventional procedures. Eachcomposition obtained was tested for stability with time at roomtemperature for one month. The results thereof are shown in Table 1.

Evaluation Criteria

Stability with time after one month storage at room temperature:

-   -   O: No solid-liquid separation was observed

X: Solid-liquid separation was observed TABLE 1 Comparative ExampleExample Ingredient (%) 1 2 3 4 1 2 3 4 Crystalline cellulose 3 3 3 3 3 33 3 (average particle diameter 4 micrometer Hydroxyethyl cellulose 1 3 11 1 1 1 1 Xanthan gum — — 1 1 — — — — Poloxamer 238 (Pluronic F88) 3 3 3— — — — — Polyoxyethylene (60 E.O.) hydrogenated — — — 3 — — — — castoroil (HCO-60) Lauryl glycoside — — — — 3 — — — Decaglycerin lauric acidester — — — — — 3 — — Sucrose lauric acid ester — — — — — — 3 — Coconutoil fatty acid amide — — — — — — — 1 propyl betaine Calcium hydrogenphosphate 30 30 30 30 30 30 30 30 Perfume 1 1 1 1 1 1 1 1 Saccharinsodium 0.1 0.1 0.1 0.1 0.1 0.1 0.1 0.1 Titanium oxide 0.3 0.3 0.3 0.30.3 0.3 0.3 0.3 Concentrated glycerin 20 20 20 20 20 20 20 20 Purifiedwater remainder remainder remainder remainder remainder remainderremainder remainder Stability with time X X X X ◯ ◯ ◯ ◯

As shown in Table 1, in Comparative Examples 1-3, the oral compositionscontaining Pluronic F88 as the surface active agent caused solid-liquidseparation even when an amount of hydroxyethyl cellulose was increased,or even when xanthan gum as another thickening agent was containedtogether. In addition, the oral composition caused solid-liquidseparation even when HCO-60 was used as the surface active agent.

On the other hand, in Examples 1-4, the oral compositions containinglauryl glycoside, polyglycerin lauric acid ester, sucrose lauric acidester or coconut oil fatty acid amide propyl betaine as the surfaceactive agent, did not cause solid-liquid separation even after one monthstorage at room temperature, which had excellent stability with time.

Example 5

An oral composition (toothpaste) of the following formulation wasprepared according to the conventional procedures: Ingredient NameAmount (%) Crystalline cellulose 3.0 (average particle diameter 3.7micrometer) Decyl glycoside 2.0 Silicic acid anhydrate 30.0 Sodiumcarboxymethyl cellulose 2.0 Tocopherol acetate 0.05 Sodium fluoride 0.2Perfume 1.0 Saccharin sodium 0.1 Titanium oxide 0.3 Sorbit solution 30.0Purified water remainder

The oral composition obtained had an excellent shape-holding ability anddispersibility in an oral cavity, did not change a taste of juice afterteeth brushing and had excellent stability with time.

Example 6

An oral composition (toothpaste) of the following formulation wasprepared according to the conventional procedures: Ingredient NameAmount (%) Crystalline cellulose 3.0 (average particle diameter 3.7micrometer) Coconut oil fatty acid amide propyl betaine 0.8 Calciumhydrogenphosphate 35.0 Cetylpyridinium chloride 0.1 Hydroxyethylcellulose 2.0 Tocopherol acetate 0.05 Sodium monofluorophosphate 0.72Perfume 1.0 Saccharin sodium 0.1 Titanium oxide 0.3 Concentratedglycerin 15.0 Purified water remainder

The oral composition obtained had an excellent shape-holding ability anddispersibility in an oral cavity, did not change a taste of juice afterteeth brushing and had excellent stability with time. In addition, theoral composition obtained had an enhanced effect of cetylpyridiniumchloride to reside on a tooth surface.

Example 7

An oral composition (toothpaste) of the following formulation wasprepared according to the conventional procedures: Ingredient NameAmount (%) Crystalline cellulose 2.0 (average particle diameter 3.7micrometer) Sucrose lauric acid ester 2.0 Calcium pyrophosphate 35.0Xanthan gum 0.5 Sodium monofluorophosphate 0.72 Perfume 1.0 Saccharinsodium 0.1 Titanium oxide 0.3 Concentrated glycerol 18.0 Polyethyleneglycol 5.0 Purified water remainder

The oral composition obtained had an excellent shape-holding ability anddispersibility in an oral cavity, did not change a taste of juice afterteeth brushing and had excellent stability with time.

Example 8

An oral composition (toothpaste) of the following formulation wasprepared according to the conventional procedures: Ingredient NameAmount (%) Crystalline cellulose 2.0 (average particle diameter 3.7micrometer) Decaglycerin lauric acid ester 2.0 Calcium carbonate 25.0Sodium carboxymethyl cellulose 1.0 Perfume 1.0 Saccharin sodium 0.1Titanium oxide 0.3 Concentrated glycerin 10.0 Xylitol 10.0 Purifiedwater remainder

The oral composition obtained had an excellent shape-holding ability anddispersibility in an oral cavity, did not change a taste of juice afterteeth brushing and had excellent stability with time.

Example 9

An oral composition (gel) of the following formulation was preparedaccording to the conventional procedures: Ingredient Name Amount (%)Crystalline cellulose 4.0 (average particle diameter 3.7 micrometer)Decyl glycoside 1.0 Sodium fluoride 0.2 Concentrated glycerin 40.0Polyethylene glycol 5.0 Propylene glycol 8.0 Perfume 1.0 Saccharinsodium 0.1 Disodium hydrogenphophate 0.12 Sodium dihydrogenphosphate0.01 Purified water remainder

The oral composition obtained had an excellent shape-holding ability anddispersibility in an oral cavity, did not change a taste of juice afterteeth brushing and had excellent stability with time.

Example 10

An oral composition (gel) of the following formulation was preparedaccording to the conventional procedures: Ingredient Name Amount (%)Crystalline cellulose 5.0 (average particle diameter 3.7 micrometer)Myristic acid amide propyl betaine 0.5 Tetraglycerin lauric acid ester1.0 Tocopherol acetate 0.1 Concentrated glycerin 30.0 Polyethyleneglycol 4.0 1,3-Butylene glycol 2.0 Perfume 1.0 Saccharin sodium 0.1Disodium hydrogencitrate 0.12 Sodium dihydrogencitrate 0.01 Purifiedwater remainder

The oral composition obtained had an excellent shape-holding ability anddispersibility in an oral cavity, did not change a taste of juice afterteeth brushing and had excellent stability with time.

Example 11

An oral composition (toothpaste) of the following formulation wasprepared according to the conventional procedures: Ingredient NameAmount (%) Crystalline cellulose 0.5 (average particle diameter 5.8micrometer) Lauryl glycoside 2.5 Calcium hydrogenphosphate dihydrate40.0 Hydroxyethyl cellulose 1.0 Perfume 1.0 Saccharin sodium 0.2Sorbitol 25.0 Purified water remainder

The oral composition obtained had an excellent shape-holding ability anddispersibility in an oral cavity, did not change a taste of juice afterteeth brushing and had excellent stability with time.

Example 12

An oral composition (toothpaste) of the following formulation wasprepared according to the conventional procedures: Ingredient NameAmount (%) Crystalline cellulose 2.0 (average particle diameter 5.8micrometer) Decyl glycoside 1.5 Silicic acid hydrate 20.0 Carrageenan1.0 Perfume 1.0 Saccharin sodium 0.1 Sorbitol 15.0 Concentrated glycerin10.0 Purified water remainder

The oral composition obtained had an excellent shape-holding ability anddispersibility in an oral cavity, did not change a taste of juice afterteeth brushing and had excellent stability with time.

Example 13

An oral composition (toothpaste) of the following formulation wasprepared according to the conventional procedures: Ingredient NameAmount (%) Crystalline cellulose 1.0 (average particle diameter 8.6micrometer) Coconut oil fatty acid amide propyl betaine 0.8 Silicic acidanhydrate 15.0 Aluminum hydroxide 5.0 Sodium polyacrylate 0.5 Perfume1.0 Saccharin sodium 0.2 Polyethylene glycol 5.0 Concentrated glycerin10.0 Purified water remainder

The oral composition obtained had an excellent shape-holding ability anddispersibility in an oral cavity, did not change a taste of juice afterteeth brushing and had excellent stability with time.

Experiment

Method of Experiment

Measurements of an Amount of Cetylpyridinium Chloride Residing onHydroxyapatite Powder

A 50 mg of hydroxyapatite (DNA Grade Bio-Gel HTP; manufactured byBIO-RAD) was immersed in 2 ml of human saliva, which had been sterilizedwith ultraviolet rays, at 37 centigrade for 15 hours to allow to form anartificial pellicle on a hydroxyapatite surface. Thereafter, a mixtureof hydroxyapatite and human saliva was centrifuged (3000 rpm, 10 min)and a supernatant was discarded. Then, residual hydroxyapatite wasimmersed at 37 centigrade for 15 minutes in 2 ml of a supernatant of afour times-diluted slurry from each of the oral compositions of Examples14-18 and Comparative Examples 5-8, in which 0.3% by weight ofcetylpyridinium chloride (CPC) and various amounts and various kinds ofthickening agents and surface active agents had been contained. Then, amixture was centrifuged (3000 rpm, 10 minutes), and a supernatant wasdiscarded. Then, 2 ml of fresh distilled water was added to the residue,the mixture was stirred and centrifuged (3000 rpm, 10 min), and thesupernatant was discarded. Again, 2 ml of fresh distilled water wasadded to the residue, the mixture was stirred and centrifuged (3000 rpm,10 minutes), and the supernatant was discarded. Next, cetylpyridiniumchloride which had adsorbed onto hydroxyapatite was extracted with anextraction solution as described below, and an amount of cetylpyridiniumchloride residing on 50 mg of hydroxyapatite was quantitatively measuredwith high performance liquid chromatography. The results thereof areshown in Table 2.

The extraction solution was prepared by mixing a solution in which 2.88g of sodium lauryl sulfate had been dissolved per 1 liter of 0.02 Mcitrate buffer, pH 3 with acetonitrile in a ratio of 1:3. TABLE 2Comparative Comparative Comparative Comparative Ingredient Example 14Example 15 Example 16 Example 17 Example 18 Ex. 5 Ex. 6 Ex. 7 Ex. 8Cetylpyridinium 0.3 0.3 0.3 0.3 0.3 0.3 0.3 0.3 0.3 chloride Crystalline4 4 4 3 3 — — — — cellulose Hydroxyethyl — — — 1 1 4 4 4 — celluloseSodium — — — — — — — — 1.5 carboxymethyl cellulose Decyl glycoside 1 — —1 — 1 — — — Lauryl glycoside — — — — 2 — — — — Coconut oil fatty — 1 — —— — 1 — 1 acid amide propyl betaine Polyoxyethylene — — 1 — — — — 1 —castor oil Calcium hydrogen 35 35 35 35 35 35 35 35 35 phosphatedihydrate Saccharin sodium 0.3 0.3 0.3 0.3 0.3 0.3 0.3 0.3 0.3 Titaniumoxide 0.3 0.3 0.3 0.3 0.3 0.3 0.3 0.3 0.3 Perfume 0.9 0.9 0.9 0.9 0.90.9 0.9 0.9 0.9 Glycerin 15 15 15 15 15 15 15 15 15 Ion exchangedremainder remainder remainder remainder remainder remainder remainderremainder remainder water CPC remaining 863 583 194 904 517 409 367 18048 amount (microgram/50 mg hydroxyapatite)

From the results in Table 2, it is found that an amount ofcetylpyridinium chloride residing on a tooth surface is significantlyincreased with the oral compositions of Examples 14-18, in whichcetylpyridinium chloride and crystalline cellulose have beenspecifically combined, as compared with those of Comparative Examples5-8, in which the same amount of cetylpyridinium chloride and othercellulose derivatives have been combined. Moreover, it is also foundthat alkyl glycoside and betaine are preferable as the surface activeagent to be contained in addition to the above ingredients, because theyincrease an amount of cetylpyridinium chloride residing on a toothsurface, as compared with other surface active agents.

Example 19

An oral composition (toothpaste) of the following formulation wasprepared according to the conventional procedures: Ingredient NameAmount (%) Benzethonium chloride 0.1 Crystalline cellulose 2.0 (averageparticle diameter 3.7 micrometer) Triclosan 0.1 Hydroxypropylmethylcellulose 1.0 Lauryl glycoside 2.0 Calcium carbonate 40.0 Titanium oxide0.2 Saccharin sodium 0.2 Sorbit solution 30.0 Perfume 1.0 Purified waterremainder

The oral composition obtained could increase an amount of the cationicbactericide residing on a tooth surface and could effectively prevent anoral cavity disease such as a periodontal disease, dental caries and thelike.

Example 20

An oral composition (toothpaste) of the following formulation wasprepared according to the conventional procedures: Ingredient NameAmount (%) Cetylpyridinium chloride 0.1 Crystalline cellulose 3.0(average particle diameter 3.7 micrometer) Potassium nitrate 1.0Hydroxyethyl cellulose 2.0 Coconut oil fatty acid amide propyl betaine1.0 Concentrated glycerin 10.0 Sorbit solution 10.0 Titanium oxide 0.3Stevioside 0.2 Sodium benzoate 0.1 Xylitol 10.0 Perfume 0.8 Purifiedwater remainder

The oral composition obtained could increase an amount of the cationicbactericide residing on a tooth surface and could effectively prevent anoral cavity disease such as a periodontal disease, dental caries and thelike.

Example 21

An oral composition (gel) of the following formulation was preparedaccording to the conventional procedures: Ingredient Name Amount (%)Cetylpyridinium chloride 0.1 Crystalline cellulose 4.0 (average particlediameter 3.7 micrometer) Decyl glycoside 1.0 Concentrated glycerin 40.0Polyethylene glycol 5.0 Propylene glycol 3.0 Perfume 1.0 Saccharinsodium 0.1 Disodium hydrogenphophate 0.12 Sodium dihydrogenphosphate0.01 Purified water remainder

The oral composition obtained could increase an amount of the cationicbactericide residing on a tooth surface and could effectively prevent anoral cavity disease such as a periodontal disease, dental caries and thelike.

Example 22

An oral composition (gel) of the following formulation was preparedaccording to the conventional procedures: Ingredient Name Amount (%)Chlorhexidine hydrochloride 0.2 Crystalline cellulose 5.0 (averageparticle diameter 3.7 micrometer) Myristic acid amide propyl betaine 0.5Tetraglycerin lauric acid ester 1.0 Tocopherol acetate 0.1 Concentratedglycerin 30.0 Polyethylene glycol 4.0 1,3-Butylene glycol 2.0 Perfume1.0 Saccharin sodium 0.1 Disodium hydrogencitrate 0.12 Sodiumdihydrogencitrate 0.01 Purified water remainder

The oral composition obtained could increase an amount of the cationicbactericide residing on a tooth surface and could effectively prevent anoral cavity disease such as a periodontal disease, dental caries and thelike.

Example 23

An oral composition (toothpaste) of the following formulation wasprepared according to the conventional procedures: Ingredient NameAmount (%) Benzalkonium chloride 0.05 Crystalline cellulose 0.5 (averageparticle diameter 5.8 micrometer) Sucrose myristic acid ester 4.0Magnesium carbonate 5.0 Calcium carbonate 12.0 Guar gum 1.0 Perfume 1.0Saccharin sodium 0.2 Concentrated glycerin 20.0 Purified water remainder

The oral composition obtained could increase an amount of the cationicbactericide residing on a tooth surface and could effectively prevent anoral cavity disease such as a periodontal disease, dental caries and thelike.

Example 24

An oral composition (gel) of the following formulation was preparedaccording to the conventional procedures: Ingredient Name Amount (%)Chlorhexidine gluconate 0.2 Crystalline cellulose 5.0 (average particlediameter 8.6 micrometer) Myristyl glycoside 4.0 Hydroxypropylmethylcellulose 1.0 Perfume 0.5 Saccharin sodium 0.2 Concentrated glycerin20.0 Propylene glycol 3.0 Purified water remainder

The oral composition obtained could increase an amount of the cationicbactericide residing on a tooth surface and could effectively prevent anoral cavity disease such as a periodontal disease, dental caries and thelike.

According to the first aspect of the present invention, an oralcomposition can be provided, which has an excellent shape-holdingability and dispersibility in an oral cavity, does not change a taste ofjuice after teeth brushing, and particularly, excellent stability withtime, or which has an enhanced ability of a cationic bactericide toreside on a tooth surface.

Moreover, according to the second aspect of the present invention, anoral composition can be provided, which can significantly increase anamount of a cationic bactericide residing on a tooth surface andeffectively prevent an oral cavity disease such as a periodontaldisease, dental caries and the like.

1. An oral composition comprising crystalline cellulose, and one or moresurface active agents selected from the group consisting of alkylglycoside, polyglycerin fatty acid ester, sucrose fatty acid ester andbetaine.
 2. The oral composition of according to claim 1, wherein thecrystalline cellulose is contained at 0.2-10% by weight.
 3. The oralcomposition according to claim 1, wherein the surface active agent isalkyl glycoside.
 4. The oral composition according to claim 3, whereinan alkyl chain of the alkyl glycoside is C8-C16 in length.
 5. The oralcomposition according to claim 1, wherein the surface active agent ispolyglycerin fatty acid ester or sucrose fatty acid ester.
 6. The oralcomposition according to claim 5, wherein an alkyl chain of a fatty acidportion of the polyglycerin fatty acid ester or the sucrose fatty acidester is C8-C16 in length.
 7. The oral composition according to claim 1,wherein the surface active agent is betaine.
 8. The oral compositionaccording to claim 7, wherein the betaine is fatty acid amide propylbetaine.
 9. The oral composition according to claim 8, wherein an alkylchain of a fatty acid portion of the fatty acid amide propyl betaine isC8-C16 in length.
 10. The oral composition according to claim 1, furthercomprising a cationic bactericide.
 11. An oral composition comprising acationic bactericide and crystalline cellulose.
 12. The oral compositionaccording to claim 11, wherein the cationic bactericide is a quaternaryammonium salt.
 13. The oral composition according to claim 11, whereinthe cationic bactericide is a biguanide bactericide.
 14. The oralcomposition according to claim 11, wherein the cationic bactericide isone or more selected from the group consisting of cetylpyridiniumchloride, benzalkonium chloride, benzethonium chloride, chlorhexidinehydrochloride and chlorhexidine gluconate.
 15. The oral compositionaccording to claim 11, wherein the cationic bactericide is contained at0.001-10% by weight.
 16. The oral composition according to claim 11,wherein the crystalline cellulose is contained at 0.2-10% by weight. 17.The oral composition according to claim 11, further comprising one ormore surface active agents selected from nonionic and amphoteric surfaceactive agents.
 18. The oral composition according to claim 17, whereinthe surface active agent is alkyl glycoside having an alkyl chain ofC8-C16 in length.
 19. The oral composition according to claim 17,wherein the surface active agent is fatty acid amide propyl betainehaving an alkyl chain of a fatty acid portion of C8-C16 in length.